Assay Detail
Binding
CHEMBL2185173
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Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid scintillation counting
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.41 | 9.40 |
| IC50 | 6 | 8.01 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL47009 | — | — | 2 | 9.40 |
| CHEMBL2177507 | — | — | 2 | 8.85 |
| CHEMBL2177508 | — | — | 2 | 8.59 |
| CHEMBL2177509 | — | — | 2 | 8.51 |
| CHEMBL2177510 | — | — | 2 | 7.66 |
| CHEMBL2177506 | — | — | 2 | 7.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL47009 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL47009 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2177507 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2177508 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2177509 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL2177507 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2177508 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2177509 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL2177510 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2177506 | — | Ki | = | 36.4 | nM | 7.44 |
| CHEMBL2177510 | — | IC50 | = | 55.9 | nM | 7.25 |
| CHEMBL2177506 | — | IC50 | = | 89.4 | nM | 7.05 |